Clinical Pharmacokinetics of Tiaprofenic Acid and its Enantiomers

@article{Davies1996ClinicalPO,
  title={Clinical Pharmacokinetics of Tiaprofenic Acid and its Enantiomers},
  author={Neal M. Davies},
  journal={Clinical Pharmacokinetics},
  year={1996},
  volume={31},
  pages={331-347}
}
  • N. Davies
  • Published 1 November 1996
  • Medicine, Biology
  • Clinical Pharmacokinetics
SummaryTiaprofenic acid is a chiral nonsteroidal anti-inflammatory drug (NSAID) of the 2-arylpropionic acid (2-APA) class. A common structural feature of 2-APA NSAIDs is a sp3-hybridised tetrahedral chiral carbon heteroatom within the propionic acid side chain moiety, with the S-enantiomer possessing most of the beneficial anti-inflammatory activity. However, all tiaprofenic acid preparations to date are marketed as the racemate. Tiaprofenic acid has been suggested to exhibit limited… 
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References

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TLDR
Results indicate that, unlike most 2-arylpropionic acid anti-inflammatory drugs, tiaprofenic acid enantiomers do not have different disposition kinetics, and the metabolic chiral inversion of one to the other does not occur or is so slow that the drug is eliminated before significant inversion takes place.
Clinical Pharmacokinetics of Flurbiprofen and its Enantiomers
  • N. Davies
  • Medicine, Biology
    Clinical pharmacokinetics
  • 1995
TLDR
Flurbiprofen binds extensively to plasma albumin, apparently in a stereoselective manner, and substantial concentrations of the drug are attained in synovial fluid, which is the proposed site of action of NSAIDs.
Clinical Pharmacokinetics of Ketoprofen and Its Enantiomers
TLDR
There appears to be circadian variation, particularly in the absorption of ketoprofen, and the relationship between concentration and anti-inflammatory effect has yet to be elucidated for this drug.
Etodolac Clinical Pharmacokinetics
TLDR
In elderly nonarthritic individuals with excellent kidney function, aging does not affect the pharmacokinetics of etodolac, and may be important because the acyl-glucuronides are renally cleared.
Pharmacokinetics of tiaprofenic acid in humans: lack of stereoselectivity in plasma using both direct and precolumn derivatization methods.
TLDR
The reported direct HPLC assay is suitable for analysis of plasma samples as reflected from small intra- and interday coefficients of variation and suitable sensitivity and the finding indicates that both direct and indirect HPLC methods are suitable for pharmacokinetic study of TA enantiomers.
Pharmacokinetics of tiaprofenic acid in healthy and arthritic subjects.
TLDR
The pharmacokinetics of tiaprofenic acid in arthritic patients seems to be similar to those in healthy subjects and under treatment with 200 mg of the drug three times daily.
Stereoselective distribution of tiaprofenic acid in synovium and cartilage in osteoarthritic patients
TLDR
Tiaprofenic acid is distributed stereoselectively in plasma and synovium, which contain a higher concentration of the active, dextrorotatory (R) enantiomer than in plasma, which reaches only a very low concentration in cartilage.
The pharmacokinetics of sustained release tiaprofenic acid in elderly arthritic patients.
TLDR
A sustained release formulation of tiaprofenic acid was given to 14 elderly arthritic patients over 4 weeks and plasma profiles obtained at the beginning and end of treatment over a 24 h period showed no evidence of any accumulation.
Human pharmacokinetics of tiaprofenic acid after regular and sustained release formulations: lack of chiral inversion and stereoselective release.
TLDR
No significant stereoselectivity was observed in the plasma concentration and urinary excretion of the enantiomers after the SR formulation, suggesting that the dissolution test at pH 8.0 better reflects the in vivo conditions, and therefore, R-TA does not undergo significant chiral inversion in humans.
Clinical Pharmacokinetics of Ketorolac Tromethamine
TLDR
Ketorolac is a new chiral nonsteroidal anti-inflammatory drug (NSAID) which is marketed for analgesia as the racemate and has a volume of distribution comparable with those of other NSAIDs.
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